Homocyclic derivatives

Details Homocyclic derivatives Homocyclic derivatives

1987-05-28

1989-02-07

Shippen, Michael L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514518, 514551, 558 37, 560173, 544154, C07C10102

Patent

active

048032018

ABSTRACT:
Aphidicolane derivatives of the formula: ##STR1## wherein R.sup.1 stands for hydrogen or a hydroxy radical, R.sup.2 stands for a hydroxy or methyl radical, or the group CR.sup.1 R.sup.2 stands for a keto group; R.sup.3 stands for a formyl or hydroxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.6, wherein R.sup.6 stands for a defined radical or R.sup.2 and R.sup.3 are joined together to form the group --O.CO.OCH.sub.2 --; R.sup.4 stands for a hydroxy radical; R.sup.5 stands for a formyl radical, a hydroxyalkyl radical --(CH.sub.2).sub.1-3 OH, a radical --CHR.sup.7 OH, wherein R.sup.7 stands for a defined radical, or R.sup.5 stands for an azidomethyl or pyrrolidinylcarbonyloxymethyl radical, or for the group --CH.sub.2 O.CO.OR.sup.8, wherein R.sup.8 stands for a defined radical, or R.sup.5 stands for the group --CH.sub.2 O.CO.(CH.sub.2).sub.m.CR.sup.11 R.sup.12.(CH.sub.2).sub.n.NR.sup.9 R.sup.10, wherein m, n, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 have defined values, or R.sup.5 stands for the group --CH.sub.2 O.SO.sub.2.R.sup.13, wherein R.sup.13 stands for a defined radical; or R.sup.4 and R.sup.5 are joined together to form the group --O.CH.sub.2 -- or --O.CO.OCH.sub.2 --; and, where appropriate, pharmaceutically-acceptable salts thereof. Processes for the preparation of said aphidicolane derivatives. Pharmaceutical compositions comprising one of the compounds and a pharmaceutical diluent or carrier. The compounds exhibit inhibitory activity against DNA-containing viruses and they inhibit the growth of some tumors.

REFERENCES:
Roche, "Design of Biopharmaceutical Properties Through Prodrugs and Analogs," pp. 27-46 & 281-315 (1977).
The Journal of Organic Chemistry, vol. 47, No. 17, Aug. 13, 1982, J. Ipsen, J. Fuska, A. Foskova and J. P. Rosazza, pp. 3278-3282, Microbial Transformations of Natural Antitumor Agents, 21. Conversions of Aphidicolin.
The Extra Pharmacopoeia, Twenty-Seventh Edition, Edited by Ainley Wade, pp. (preface) XIV-XV.

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